Guaiphenesin
Guaiphenesin Uses, Dosage, Side Effects, Food Interaction and all others data.
Guaiphenesin possesses a storied history, having been originally formally approved by the US FDA in 1952 and continues to be one of very few - if not perhaps the only drug that is readily available and used as an expectorant . Since that time the agent has been a combination component of various prescription and non-prescription over-the-counter cough and cold products and is currently a widely available over-the-counter generic medication . Although it is principally believed that guaifenesin elicits an action to facilitate productive cough to manage chest congestion , it is not known whether the agent can reliably mitigate coughing.
Regardless, on March 1, 2007, the FDA received a petition asking the FDA to notify the public that some antitussives, expectorants, decongestants, antihistamines, and cough/cold combinations are not known to be safe and effective in children under the age of 6 years . After the negotiation between FDA and major manufacturers, a voluntary transition of labels for not using guaifenesin in children under the age of 4 years was endorsed by FDA in 2008 .
Furthermore, there has also been contemporary research to suggest that guaifenesin possesses and is capable of demonstrating anticonvulsant and muscle relaxant effects to some degree possibly by acting as an NMDA receptor antagonist .
| Trade Name | Guaiphenesin |
| Availability | Rx and/or OTC |
| Generic | Guaifenesin |
| Guaifenesin Other Names | Glyceryl guaiacolate, Guaifenesin, Guaifenesina, guaiphenesin |
| Related Drugs | amoxicillin, albuterol, doxycycline, ciprofloxacin, azithromycin, ceftriaxone, levofloxacin, diphenhydramine, Benadryl, benzonatate |
| Type | |
| Formula | C10H14O4 |
| Weight | Average: 198.2158 Monoisotopic: 198.089208936 |
| Protein binding | Information regarding the protein binding of guaifenesin is not readily available or accessible. |
| Groups | Approved, Investigational, Vet approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Guaiphenesin is an expectorant commonly found in OTC products for the symptomatic relief from congested chests and coughs associated with cold, bronchitis, and/or other breathing illnesses.
Guaiphenesin is an expectorant that is indicated for providing temporary symptomatic relief from congested chests and coughs which may be due to a cold, bronchitis, and/or other breathing illnesses .
Guaiphenesin is also used to associated treatment for these conditions: Allergic Reaction, Asthma, Asthma, Allergic, Bronchial Asthma, Bronchitis, Bronchospasm, Chronic Bronchitis, Chronic Obstructive Respiratory Diseases, Common Cold, Cough, Cough caused by Common Cold, Coughing caused by Allergies, Coughing caused by Flu caused by Influenza, Drug Allergy, Emphysema, Fever, Flu caused by Influenza, Food Allergy, Headache, House dust allergy, Irritative cough, Laryngitis, Nasal Congestion, Nasal Congestion caused by Common Cold, Phlegm, Pollen Allergy, Productive cough, Rash, Rhinorrhoea, Sneezing, Sore Throat, Tracheitis, Urticaria, Whooping Cough, Acute Rhinitis, Chest congestion, Chills occurring with fever, Dry cough, Excess mucus or phlegm, Mild to moderate pain, Minor aches and pains, Airway secretion clearance therapy, Expectorant
How Guaiphenesin works
Although the exact mechanism of action of guaifenesin may not yet be formally or totally elucidated, it is believed that expectorants like guaifenesin function by increasing mucus secretion . Moreover, it is also further proposed that such expectorants may also act as an irritant to gastric vagal receptors, and recruit efferent parasympathetic reflexes that can elicit glandular exocytosis that is comprised of a less viscous mucus mixture . Subsequently, these actions may provoke coughing that can ultimately flush difficult to access, congealed mucopurulent material from obstructed small airways to facilitate a temporary improvement for the individual .
Consequently, while it is generally proposed that guaifenesin functions as an expectorant by helping to loosen phlegm (mucus) and thin bronchial secretions to rid the bronchial passageways of bothersome mucus and make coughs more productive, there has also been research to suggest that guaifenesin possesses and is capable of demonstrating anticonvulsant and muscle relaxant effects to some degree possibly by acting as an NMDA receptor antagonist .
Toxicity
The most prevalent signs and symptoms associated with an overdose of guaifenesin have been nausea and vomiting .
Although adequate and well-controlled studies in pregnant women have not been performed, the Collaborative Perinatal Project monitored 197 mother-child pairs exposed to guaifenesin during the first trimester . An increased occurrence of inguinal hernias was found in the neonates . However, congenital defects were not strongly associated with guaifenesin use during pregnancy in 2 large groups of mother-child pairs .
Moreover, guaifenesin is excreted in breast milk in small quantities . Subsequently, caution should be exercised by balancing the potential benefit of treatment against any possible risks .
Additionally, an LD50 value of 1510 mg/kg (rat, oral) has been reported for guaifenesin .
Food Interaction
- Take with a full glass of water.
- Take with or without food. The absorption is unaffected by food.
Volume of Distribution
The geometric mean apparent volume of distribution of guaifenesin determined in healthy adult subjects is 116L (CV=45.7%) .
Elimination Route
Studies have shown that guaifenesin is well absorbed from and along the gastrointestinal tract after oral administration .
Half Life
The half-life in plasma observed for guaifenesin is approximately one hour .
Clearance
The mean clearance recorded for guaifenesin is about 94.8 L/hr (CV=51.4%) .
Elimination Route
After administration, guaifenesin is metabolized and then largely excreted in the urine .
Innovators Monograph
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